Heteroaryl butanoic acid derivatives
AssigneeNovartis AG
InventorsBirgit Bollbuck, Christian Markert, Wolfgang Miltz, Till Roehn
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Abstract
The present invention describes novel heteroaryl butanoic acid derivatives that are good drug candidates especially with regard to leukotriene A4 hydrolase (LTA4H). The present invention also relates to pharmaceutical compositions comprising said novel heteroaryl butanoic acid derivatives, methods of using said compounds in the treatment of various diseases and disorders, and processes for preparing the said novel compounds.
Claims31
A method of modulating leukotriene A4 hydrolase (LTA4H) activity in a subject, wherein the method comprises administering to the subject a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof;
- wherein,
- R1 is OH or NH2;
- Y is O, S or CH2;
- X1, X2, X3 and X4 are N;
- or
- X1, X2, X3 and X4 are selected from N, NH, C, CH and O with the proviso that at least two of X1, X2, X3 or X4 are N or NH;
- R2 is C1-C6 alkyl optionally substituted by phenyl;
- C3-C6 cycloalkyl;
- phenyl optionally being substituted by halogen, cyano, C1-C6 alkyl optionally substituted by halogen, C1-C6 alkoxy, or a 5-6 membered heteroaryl ring containing 1 to 3 heteroatoms selected from N, O and S;
- or a 5-10 membered mono- or bicyclic heteroaryl containing 1 to 4 heteroatoms selected from N, O and S, said heteroaryl being optionally substituted by halogen, cyano or C1-C6 alkyl optionally substituted by halogen.
A method of treating a disease or disorder associated with leukotriene A4 hydrolase (LTA4H) activity, wherein the method comprises administering to a subject a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof;
- wherein,
- R1 is OH or NH2;
- Y is O, S or CH2;
- X1, X2, X3 and X4 are N;
- or
- X1, X2, X3 and X4 are selected from N, NH, C, CH and O with the proviso that at least two of X1, X2, X3 or X4 are N or NH;
- R2 is C1-C6 alkyl optionally substituted by phenyl;
- C3-C6 cycloalkyl;
- phenyl optionally being substituted by halogen, cyano, C1-C6 alkyl optionally substituted by halogen, C1-C6 alkoxy, or a 5-6 membered heteroaryl ring containing 1 to 3 heteroatoms selected from N, O and S;
- or a 5-10 membered mono- or bicyclic heteroaryl containing 1 to 4 heteroatoms selected from N, O and S, said heteroaryl being optionally substituted by halogen, cyano or C1-C6 alkyl optionally substituted by halogen,
- and wherein the disease or disorder is selected from acute or chronic inflammation, anaphylactic reactions, allergic reactions, atopic dermatitis, psoriasis, acute respiratory distress syndrome, immune complex-mediated pulmonary injury and chronic obstructive pulmonary disease, inflammatory bowel diseases, gastrointestinal ulcers, neutrophilic dermatoses, immune-complex-mediated glomerulonephritis, autoimmune diseases, vasculitides, cardiovascular disorders, sepsis, inflammatory, neuropathic pain, arthritic pain, periodontal disease, ear infections, migraine, benign prostatic hyperplasia, Sjogren-Larsson Syndrome and cancers.
Dependencies are inferred from the claim text.